Patent classifications
C07C271/16
High penetration drugs and their compositions thereof for treatment of Parkinson diseases
One aspect of the invention provides a composition of novel high penetration compositions (HPC) or a high penetration prodrug (HPP) for treatment of Parkinson's disease. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
BRANCHED TYPE HETERO MONODISPERSED POLYETHYLENE GLYCOL, PRODUCTION METHOD THEREOF, AND CONJUGATE THEREOF
An intermediate for production of a branched type hetero monodispersed polyethylene glycol which is represented by formula (2), the intermediate being represented by formula (3) or (40):
##STR00001##
where X.sup.1, L.sup.1, L.sup.3, Y.sup.1, Y.sup.2, and n are as defined herein.
CATIONIC LIPID
The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R.sup.1 and R.sup.2 are, the same or different, alkenyl, etc, and X.sup.1 and X.sup.2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X.sup.3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L.sup.3 is a single bond, etc, R.sup.3 is alkyl, etc, L.sup.1 and L.sup.2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
##STR00001##
CATIONIC LIPID
The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R.sup.1 and R.sup.2 are, the same or different, alkenyl, etc, and X.sup.1 and X.sup.2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X.sup.3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L.sup.3 is a single bond, etc, R.sup.3 is alkyl, etc, L.sup.1 and L.sup.2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.
##STR00001##
CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
A chemical blowing agent is described that includes at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can, for example, be incorporated into thermally expandable baffle and/or reinforcement elements, which can be used in automotive manufacturing and building insulation.
CHEMICAL BLOWING AGENT AND THERMALLY EXPANDABLE THERMOPLASTIC COMPOSITION
A chemical blowing agent is described that includes at least one tertiary alkyl carbamate. The chemical blowing agent can be activated thermally and is suitable for foaming thermoplastic materials and can, for example, be incorporated into thermally expandable baffle and/or reinforcement elements, which can be used in automotive manufacturing and building insulation.
Preparation method of supercritical carbon dioxide thickener for tight oil and gas reservoir
The present invention disclosed a method for preparing a thickener for tight oil and gas reservoir, which relieves damages. The technical solution includes the following steps: putting a three-flask in ice; adding perfluoroalkyl alcohol, P-toluenesulfonyl chloride and pyridine; reacting for 3 h at 0-20° C.; adding filter paper; ultrasonic dispersing for 1 h; removing the filter paper; washing the solution for 3-5 times by adding dilute hydrochloric acid to collect the intermediate product (I); adding 1,3-dihydroxy-propane-2-tert-butyl carbamate and the intermediate product (I) in another three-flask; adding potassium carbonate and N,N-dimethylformamide; reacting for 4 h at 40° C. to collect the intermediate product (II); adding trifluoroacetic acid and methylene chloride into the intermediate product (II); reacting at 45° C. for 2 h; extracting and vacuum drying; and adding 1,6-hexamethylene diisocyanate; reacting for 2 h to collect the final product (III).
Preparation method of supercritical carbon dioxide thickener for tight oil and gas reservoir
The present invention disclosed a method for preparing a thickener for tight oil and gas reservoir, which relieves damages. The technical solution includes the following steps: putting a three-flask in ice; adding perfluoroalkyl alcohol, P-toluenesulfonyl chloride and pyridine; reacting for 3 h at 0-20° C.; adding filter paper; ultrasonic dispersing for 1 h; removing the filter paper; washing the solution for 3-5 times by adding dilute hydrochloric acid to collect the intermediate product (I); adding 1,3-dihydroxy-propane-2-tert-butyl carbamate and the intermediate product (I) in another three-flask; adding potassium carbonate and N,N-dimethylformamide; reacting for 4 h at 40° C. to collect the intermediate product (II); adding trifluoroacetic acid and methylene chloride into the intermediate product (II); reacting at 45° C. for 2 h; extracting and vacuum drying; and adding 1,6-hexamethylene diisocyanate; reacting for 2 h to collect the final product (III).
Branched Discrete PEG Constructs
Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line,
, having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.
Branched Discrete PEG Constructs
Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line,
, having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.